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醋丁洛尔和双醋洛尔在人体中的血浆蛋白结合情况。

Blood plasma binding of acebutolol and diacetolol in man.

作者信息

Coombs T J, Coulson C J, Smith V J

出版信息

Br J Clin Pharmacol. 1980 Apr;9(4):395-7. doi: 10.1111/j.1365-2125.1980.tb01067.x.

Abstract

1 Acebutolol or diacetolol were added to fresh human plasma in varying concentrations and their extent of binding at 25 degrees C measureed by an equilibrium dialysis technique. 2 The extent of binding for both compounds was shown to be very low, being 11-19% for acebutolol and 6-9% for diacetolol. 3 Partition coefficients were measured in an n- octanol/phosphate buffer (0.05M, pH 7.4) solvent system. For a cebutolol, P = 0.62 and for diacetol, P = 0.08. 4 The very low plasma binding is in accord with the hydrophilic partition coefficients of these compounds.

摘要
  1. 将醋丁洛尔或双醋洛尔以不同浓度添加到新鲜人血浆中,并通过平衡透析技术测定它们在25℃时的结合程度。2. 结果表明,两种化合物的结合程度都非常低,醋丁洛尔为11 - 19%,双醋洛尔为6 - 9%。3. 在正辛醇/磷酸盐缓冲液(0.05M,pH 7.4)溶剂系统中测量分配系数。醋丁洛尔的P = 0.62,双醋洛尔的P = 0.08。4. 极低的血浆结合与这些化合物的亲水性分配系数一致。

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Biochem Soc Trans. 1975;3(5):635-40. doi: 10.1042/bst0030635.
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Clin Pharmacol Ther. 1977 Nov;22(5 Pt 1):557-67. doi: 10.1002/cpt1977225part1557.
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Equilibrium dialysis: a new approach.平衡透析:一种新方法。
Biochem Soc Trans. 1978;6(5):1048-50. doi: 10.1042/bst0061048.
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Suppression of premature ventricular contractions by acebutolol.
Circulation. 1977 May;55(5):785-91. doi: 10.1161/01.cir.55.5.785.

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